Osilodrostat

一种醛固酮合成酶抑制剂；对人醛固酮合成酶的选择性高于大鼠醛固酮合成酶（IC₅₀=160nM）；能够抑制由血管紧张素II或ACTH诱导的大鼠血浆醛固酮水平升高（ED₅₀分别为0.6mg/kg和1.1mg/kg）；在表达人肾素和血管紧张素原的双转基因大鼠模型中，以剂量依赖性方式降低平均动脉压并延长生存期，该模型是一种血管紧张素II依赖性高血压模型。An aldosterone synthase inhibitor; selective for human aldosterone synthase over rat aldosterone synthase (IC50 = 160 nM); inhibits increases in plasma aldosterone levels induced by angiotensin II or ACTH in rats (ED50s = 0.6 and 1.1 mg/kg, respectively); reduces mean arterial pressure and prolongs survival in rats expressing human renin and angiotensinogen, a double-transgenic model of angiotensin II-dependent hypertension, in a dose-dependent manner.分子式C13H10FN3分子量227.2FC1=C(C=CC(C#N)=C1)[C@]2([H])N3C(CC2)=CN=C3